PF-00337210, a potent, selective and orally bioavailable small molecule inhibitor of VEGFR-2

@inproceedings{Marrone2007PF00337210AP,
  title={PF-00337210, a potent, selective and orally bioavailable small molecule inhibitor of VEGFR-2},
  author={Tami Marrone and Dana D. Hu-Lowe and Maren L. Grazzini and Min-Jean Yin and Jeffrey H. Chen and Max Hallin and Karin Kristina Amundson and Shinji Yamazaki and David Romero and Aileen McHarg and Eileen R. Blasi and Yufeng Hong and Eileen Valenzuela Tompkins and Theodore Johnson and Judith Gail Deal and Brion William Murray and James Solowiej and Michele A McTigue and John A. Wickersham and Steven Lee Bender},
  year={2007}
}
3992 PF-00337210 is a potent, selective, and orally bioavailable small molecule inhibitor of VEGFRs. It is an ATP-competitive compound that is selective for VEGFR-2 when biochemically profiled against >100 diverse tyrosine and serine-threonine kinases. PF-00337210 preferentially binds to the unactivated kinase (Ki=0.7 nM) relative to the fully phosphorylated form (Ki= 8.8 nM). Crystallographic evidence suggests that its selectivity is likely a result of its ability to bind to a DFG-out… CONTINUE READING